Bioavailability Enhancement: The Process How To Decide Which Approach To Take

CoreRx East

The process of turning a low bioavailability drug into a viable therapy begins by looking at the physical properties of the active ingredient. Data on thermal properties, particle size distribution, morphology, and other factors can yield insights into which method will deliver the best results. CoreRx then runs various analyses evaluating chemical properties of the substance including assay, related compounds, intrinsic dissolution in various media, and molecular stability. The third critical piece of information is the targeted level of bioavailability. If animal studies have shown that a threefold rise in bioavailability is needed, the team will focus on both physical and chemical methods that can achieve this goal.

Once the team understands the active’s characteristics, it chooses bioavailability enhancement techniques from one of three broad categories: physical, chemical, and complexation. Physical modifications include micronization, solid state dispersion, and creation of nanoparticles. If the team decides a chemical modification would work better, a change in pH, use of a buffer, or different salt form of the molecule might be considered with the client. In other instances, CoreRx uses complexation — a growing approach that combines the molecule with other agents such as cyclodextrins or hydrophobic materials — which can have a dramatic effect on both solubility and bio enhancement.

Many clients want the same thing: a high-energy amorphous state of their molecule. The challenge is working out the most effective, efficient way to achieve this goal. A skilled team will know which approach to use and have proprietary technologies that deliver the best possible outcome.

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